Date: 2013-10-25
Type of information: R&D agreement
Compound: DNX-04042
Company: CleveXel Pharma (France) Dynamix Pharmaceuticals (Israel)
Therapeutic area: Autoimmune diseases – Inflammatory diseases - Rheumatic diseases
Type agreement: R&D
development
Action mechanism: SYK and JAK3 are intracellular tyrosine kinases involved in cytokine and antibody receptor signaling. JAK3, which is a member of the JAK family, is frequently activated during the course of inflammatory autoimmune diseases. However, unlike JAK1 which is ubiquitously expressed and JAK2 which is prominent in erythrocytes, JAK3 is predominantly expressed in immune cells (B- and T-cells) making it a promising target for treating autoimmune diseases and hematological malignancies. SYK is a key kinase in B-cell signaling. DNX-04042 is a potent, oral, small-molecule inhibitor of both SYK and JAK3 with significant selectivity within the JAK-family and across the kinome. Specifically, DNX-04042 exhibits more than 1,500 fold selectivity in cells for JAK3 over JAK2 inhibition. DNX-04042 has a promising pharmacological profile and has demonstrated excellent safety in a preclinical MTD study. DNX-04042 has also demonstrated a very strong anti-cancer effect in a mouse xenograft study of B-cell lymphoma.
Disease: rheumatoid arthritis
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